1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. SKLB4771

SKLB4771 (Synonyms: FLT3-​IN-​1)

Cat. No.: HY-12960 Purity: ≥98.0%
Handling Instructions

SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.

For research use only. We do not sell to patients.

SKLB4771 Chemical Structure

SKLB4771 Chemical Structure

CAS No. : 1370256-78-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 248 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 248 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
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Description

SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM. IC50 value: 10 nM (in vitro) [1] Target: in vitro: SKLB4771 inhibited FLT3 phosphorylation in a dose-dependent manner. Consistent with the downregulation of the phosphorylation of FLT3, the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM. SKLB4771 potently inhibited the growth of MV4-11 cells that express FLT3-ITD, with an IC50 value of 0.006 μM. It just exhibited very weak inhibitory activity against human T lymphoma Jurkat cells, human Burkitt's lymphoma Ramos cells, human lung cancer PC-9 and H292 cells, and human epithelial carcinoma A431 cells (IC50: 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM, and 8.91 μM, respectively). For other leukemia and solid tumor cell lines, including K562, U937, Karpas299, HCC827, A549, H2228, H820, MDA-MB-231, BT474, MCF-7, HCT116, SW480, LoVo, HeLa, SKOV-3, SK, DU145, PC-3, A431, and SH-SY5Y [1]. in vivo: Treatment with SKLB4771 at 100 mg/kg/d resulted in rapid and complete tumor regression in all mice of this group. SKLB4771 treatment at 20 mg/kg/d and 40 mg/kg/d significantly slowed down the tumor growth; the tumor inhibition rates are 66% and 84%, respectively. Moreover, during the whole experiment, no significant weight loss or any other obvious signs of toxicity were observed for all of the SKLB4771 treated mice.

Molecular Weight

537.66

Formula

C25H27N7O3S2

CAS No.
SMILES

O=C(NC1=NN=C(SC2=C3C=CC(OCCCN4CCOCC4)=CC3=NC=N2)S1)NC5=CC=C(C)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (61.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8599 mL 9.2996 mL 18.5991 mL
5 mM 0.3720 mL 1.8599 mL 3.7198 mL
10 mM 0.1860 mL 0.9300 mL 1.8599 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Product Name:
SKLB4771
Cat. No.:
HY-12960
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